Abstract |
In recent years, there has been an increased effort in the development of therapies which target an epigenetic mode of action. Among thes e efforts include progress in the development of inhibitors of EZH2 ( Enhancer of Zeste Homolog 2), a key epigenetic target with strong disease implications to cancer. Over the last 3+ years, multiple reports describing small molecule inhibitors of EZH2 have been described, including those for chemical probes and drug candidates which have entered the clinic as first-in-class agents. Recent progress in this emerging area is presented in this review.
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Authors | Sharad K Verma |
Journal | Current topics in medicinal chemistry
(Curr Top Med Chem)
Vol. 15
Issue 8
Pg. 714-9
( 2015)
ISSN: 1873-4294 [Electronic] United Arab Emirates |
PMID | 25732793
(Publication Type: Journal Article, Review)
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Chemical References |
- Antineoplastic Agents
- Enzyme Inhibitors
- EZH2 protein, human
- Enhancer of Zeste Homolog 2 Protein
- Polycomb Repressive Complex 2
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Topics |
- Antineoplastic Agents
(pharmacology)
- Enhancer of Zeste Homolog 2 Protein
- Enzyme Inhibitors
(pharmacology)
- Epigenesis, Genetic
- Gene Expression Regulation, Neoplastic
- Humans
- Polycomb Repressive Complex 2
(antagonists & inhibitors, genetics, metabolism)
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